Teneligliptin [chemical name: {(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]-pyrrolidin-2-yl}(1,3-thiazolidin-3-yl)methanone] is a compound represented by the formula (I):
and 5/2 hydrobromide.hydrate thereof is under clinical development as a therapeutic drug for type 2 diabetes, based on a potent and sustained dipeptidyl peptidase-IV inhibitory action.
As a formulation or production method of a solid preparation containing teneligliptin or a salt thereof, or a solvate thereof (hereinafter sometimes to be abbreviated as a teneligliptin-containing solid preparation), it is known that teneligliptin or a salt thereof, or a solvate thereof and a conventional carrier for medicaments are mixed and formulated (see patent documents 1 and 2).
The present inventors have produced a teneligliptin-containing solid preparation having a conventional pharmaceutical formulation for production of a solid preparation, and investigated the quality of the preparation. As a result, they have confirmed that a long-term preservation of a teneligliptin-containing solid preparation having a particular content for about several months causes delayed dissolution of teneligliptin or a salt thereof, or a solvate thereof, which is the active ingredient.
While an influence of such delay in the dissolution over time of the active ingredient on the efficacy of a pharmaceutical product is not easy to predict accurately, a preparation showing a stable dissolution behavior is considered to be more preferable as a pharmaceutical product.